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| | Pimobendan Basic information |
| | Pimobendan Chemical Properties |
| Melting point | approximate 243℃ (dec.) | | density | 1.36 | | storage temp. | 2-8°C | | solubility | DMSO: soluble5mg/mL, clear (warmed) | | form | powder | | pka | 10.55±0.10(Predicted) | | color | white to beige | | InChI | InChI=1S/C19H18N4O2/c1-11-9-17(24)22-23-18(11)13-5-8-15-16(10-13)21-19(20-15)12-3-6-14(25-2)7-4-12/h3-8,10-11H,9H2,1-2H3,(H,20,21)(H,22,24) | | InChIKey | GLBJJMFZWDBELO-UHFFFAOYSA-N | | SMILES | C1(=O)NN=C(C2C=C3NC(C4=CC=C(OC)C=C4)=NC3=CC=2)C(C)C1 | | CAS DataBase Reference | 74150-27-9(CAS DataBase Reference) |
| RIDADR | UN 2811 6.1 / PGIII | | HS Code | 2933995300 |
| | Pimobendan Usage And Synthesis |
| Description | Pimobendan, a novel cardiotonic vasodilator, was introduced in Japan for the
treatment of acute and mild to moderate chronic heart failure. It is a
phosphodiesterase Ⅲ inhibitor and is able to enhance sensitization of myocardial
contractile regulatory protein to calcium ions. The combination of these effects
contribute to its inotropic activity. In patients with severe congestive heart failure,
orally administered pimobendan improves cardiac index, stroke volume index,
pulmonary wedge pressure, and systemic and pulmonary vascular resistance.
Pimobendan is reported to be well tolerated and largely devoid of the proarrhythmic
effects of classical phosphodiesterase Ill inhibitors. Studies also suggested that
combination of the inotropic agent pimobendan with an ACE inhibitor such as
enalapril may be superior to monotherapy for heart failure patients. | | Chemical Properties | White Solid | | Originator | Boehringer
lngelhelm (Germany) | | Uses | Pimobendan is a cardiotonic agent. The study of the cardiotonic mechanism of Pimobendan using ventricular muscles from rabbits and guinea pigs suggests that Pimobendan acts by inhibiting phosphodiesterase III and potassium channel. The potent venodilating action of Pimobendan makes it a suitable treatment option for patients with congestive heart failure (CHF) as it also improves systemic vasoconstriction. | | Uses | Pimobendan is a selective inhibitor of PDE3 with IC50 of 0.32 μM. It is a drug with both inotropic and vasodilatory properties that is used for the treatment of var-ious cardiac diseases. | | Definition | ChEBI: Pimobendan is a pyridazinone and a member of benzimidazoles. It has a role as a cardiotonic drug, a vasodilator agent and an EC 3.1.4.* (phosphoric diester hydrolase) inhibitor. | | Brand name | Acardl | | Biological Activity | Pimobendan is an inhibitor of phosphodiesterase 3 (PDE3; IC50 = 0.32 μM for guinea pig cardiac enzyme) that is selective for PDE3 over PDE1, PDE2, and PDE4 (IC50s = >30 μM). It is also a calcium sensitizer, decreasing the concentration of calcium required for half-maximal contractile force in isolated, skinned porcine ventricular fibers. Pimobendan increases the force of contraction in electrically-stimulated isolated guinea pig papillary muscles with an EC50 value of 6 μM, indicating positive inotropic effects. It increases survival time in dogs with congestive heart failure due to myxomatous mitral valve disease when administered in combination with angiotensin-converting enzyme inhibitors and furosemide . Formulations containing pimobendan have been used in the treatment of heart failure in dogs. | | Biochem/physiol Actions | Pimobendan is an inotropic agent with a dual mechanism of action: it increases myocardial contractility by increasing calcium sensitization to troponin C and it promotes vasodilation by inhibiting phosphodiesterase III (PDE3). Pimobendan has been studied for treating heart failure and cardiomyopathy, primarily for veterinary uses. | | Veterinary Drugs and Treatments | Pimobendan is used to treat dogs with congestive heart failure secondary
to dilated cardiomyopathy or chronic mitral valve insufficiency
(CMVI). |
| | Pimobendan Preparation Products And Raw materials |
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